| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
STAT3
Golotimod targets STAT3 (signal transducer and activator of transcription 3), a transcription factor involved in various cellular processes including immunity, inflammation, and cancer. By inhibiting STAT3 homodimerization in the cytoplasm, the compound blocks STAT3 signaling. The compound also exhibits antibacterial activity, suggesting additional targets in bacterial pathogens. |
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| ln Vitro |
Golotimod hydrochloride demonstrates in vitro antibacterial activity. It inhibits STAT3 signaling by blocking STAT3 homodimerization in the cytoplasm. The compound stimulates thymic and splenic cell proliferation and improves macrophage phagocytosis activity. Its immunomodulatory activity makes it a valuable tool for studying immune responses.
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| ln Vivo |
Golotimod (SCV-07) hydrochloride, administered orally (oral gavage or subcutaneous injection, 100 μg/kg, 5 days), decreases experimental recurrent genital HSV-2 disease. Moreover, oral SCV-07 administered after fasting significantly lowers incidence and severity in female Hartley guinea pigs compared to SCV-07 administered without fasting[1]. In male LVG golden Syrian Hamsters, golotimod (SCV-07) hydrochloride (subcutaneous injection, once or twice a day, 100 μg/kg) can shorten the length of ulcerative OM and lessen the intensity and duration of acute and split radiation-induced oral mucositis (OM)[3].
In vivo activity of golotimod hydrochloride has been demonstrated in animal models. It modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation. It significantly increases the efficacy of anti-tuberculosis therapy. It is a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2). |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for golotimod hydrochloride involve measuring its inhibition of STAT3 homodimerization. The assay typically uses purified STAT3 protein or cell lysates and measures the formation of STAT3 dimers in the presence of the compound. Inhibition of STAT3 signaling can be assessed by measuring STAT3 phosphorylation or downstream target gene expression.
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| Cell Assay |
In vitro cellular assays for golotimod hydrochloride involve treating immune cells (e.g., macrophages, splenic cells) with varying concentrations of the compound. Immunomodulatory activity is assessed by measuring cell proliferation, phagocytosis activity, and cytokine production. Antibacterial activity is assessed using standard bacterial growth inhibition assays.
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| Animal Protocol |
Animal/Disease Models: Female Hartley guinea pigs (250-300 g) infected HSV-2[1]
Doses: 100 μg/kg Route of Administration: po (oral gavage) or subcutaneous (sc)injection; 5 days Experimental Results: diminished incidence of lesions from 55% (one week before treatment) to only 18% by oral administration, and demonstrated no significant reduction in disease by subcutaneous (sc)injection of SCV-07. Animal/Disease Models: Male LVG golden Syrian Hamsters weighing approximately 80 g with radiation-induced mucositis[3] Doses: 10, 100 μg/kg or 1 mg/kg Route of Administration: subcutaneous (sc)injection; once or twice a day from days 1 to 20 Experimental Results: demonstrated a peak mucositis of 3.0 on day 18 in the control group compared to only 2.2 in the test group, and the mucositis score in the SCV-07 treated hamsters was only 6.3% compared to 28.1% in the control group at dose of 100 μg/kg. Dramatically diminished the severity and duration of oral mucositis (OM) at dose of 10 μg/kg, 100 μg/kg or 1 mg/kg. In vivo animal experiments for golotimod hydrochloride involve administering the compound to animal models of oral mucositis, tuberculosis, or HSV-2 infection. Efficacy is evaluated by measuring disease severity, bacterial load, immune cell function, or clinical outcomes. The compound's immunomodulatory effects are assessed by measuring immune cell populations and cytokine levels. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for golotimod hydrochloride indicate that it has a molecular weight of 369.80 and appears as a solid. Purity is 99.79%. Its absorption, distribution, metabolism, and excretion properties have not been fully characterized. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
Toxicological data for golotimod hydrochloride are limited. As a research compound, comprehensive toxicological studies have not been reported. The compound is intended for research use only and is not for human therapeutic application. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
Golotimod hydrochloride (SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride) (CAS#: 1029401-59-9) has the molecular formula C16H20ClN3O5 and a molecular weight of 369.80. It is an immunomodulatory peptide with antibacterial activity that inhibits STAT3 signaling. Purity is 99.79%. It is for research use only.
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| Molecular Formula |
C16H20CLN3O5
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|---|---|
| Molecular Weight |
369.800103187561
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| Exact Mass |
369.109
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| CAS # |
1029401-59-9
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| Related CAS # |
Golotimod;229305-39-9;Golotimod TFA;2828433-07-2
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| PubChem CID |
154805962
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
25
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| Complexity |
484
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC=C2C(=C1)C(=CN2)CC(C(=O)O)NC(=O)CC[C@H](C(=O)O)N.Cl
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| InChi Key |
YYTBHYZPAMPQGT-ZRMPQGGQSA-N
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| InChi Code |
InChI=1S/C16H19N3O5.ClH/c17-11(15(21)22)5-6-14(20)19-13(16(23)24)7-9-8-18-12-4-2-1-3-10(9)12;/h1-4,8,11,13,18H,5-7,17H2,(H,19,20)(H,21,22)(H,23,24);1H/t11-,13?;/m1./s1
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| Chemical Name |
(2R)-2-amino-5-[[1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-5-oxopentanoic acid;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : 150 mg/mL (405.62 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 20 mg/mL (54.08 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7042 mL | 13.5208 mL | 27.0416 mL | |
| 5 mM | 0.5408 mL | 2.7042 mL | 5.4083 mL | |
| 10 mM | 0.2704 mL | 1.3521 mL | 2.7042 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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